(315f) Evaluation of Vegetarian Softgels Using SeaGel® Technology for Pharmaceutical Applications

Softgels continuously serve as a preferred oral drug and dietary supplement dosage forms. As softgels can easily encapsulate a variety of liquid and semi-solid formulations, they have been used to deliver poorly soluble active ingredients and provide enhanced bioavailability. Although gelatin softgels currently dominate the pharmaceutical industry, there are numerous shortcomings with the material. Gelatin has the potential to crosslink with active ingredients leading to reduced solubility of the capsule shell. Gelatin is sensitive to high temperature and humidity conditions, presenting challenges with storage and shipment of gelatin softgels. There is also a growing consumer preference for non-animal products to suit different dietary needs (vegan, halal, kosher, etc). In this study, a poorly soluble active pharmaceutical ingredient (API), Ibuprofen, was encapsulated using either gelatin as the shell forming material or a plant-based material based on IFF’s SeaGel^® technology (noted as SeaGel^® softgels).

This study used the USP I method to study the dissolution behavior of Ibuprofen from gelatin and SeaGel® capsules. Additionally, evaluation of stability of both gelatin softgels and SeaGel® softgels was performed at accelerated storage conditions (40 ⁰C, 75% RH) as well as long term storage conditions (30 ⁰C, 65% RH) for more than 2 months.

For freshly produced SeaGel and gelatin softgels, it was observed that the plant based SeaGel^® softgels have slightly slower delivery at dissolution time less than 80 minutes. However, the f₂ similarity factor was greater than 52 at all time points which indicates an average difference of less than 10% between SeaGel softgels and gelatin softgels. Additionally, when stored at accelerated or long term storage condition for more than 1 month, SeaGel® softgels showed equivalent dissolution profile as the profile of freshly produced SeaGel softgels, while gelatin softgels showed significantly slower dissolution behavior than its profile of freshly produced gelatin softgels. Furthermore, the mechanical properties of gelatin softgels indicated possible cross-linking and migration of fill components and varies more significantly than those of SeaGel^® softgels as a function of aging time and aging conditions. This is consistent with similar findings of other scientists. ¹

In summary, dissolution of an active in the dosage form is critical for absorption and bioavailability, and for product quality and consistency assessments during drug product life cycle. SeaGel^® softgels showed approximately equivalent API dissolution behavior as that of gelatin capsules at the time of capsules were produced but better stability than that of gelatin softgels.

References

1. Chen, T. Humidity Influence to the Thermal and

Mechanical Properties of Gelatin Capsules. https://www.tainstruments.com/pdf/literature/TA409.pdf.